Histatin 5 suppresses the activities of matrix metalloproteinases MMP-2 and MMP-9 with IC50 values of 0.57 and 0.25μM, respectively[1]. Histatin 5 significantly inhibited the growth of a variety of Candida species by binding to Candida cell wall proteins (Ssa1/2) and glycans with MIC50 values of 10-20μg/ml[2]. Histatin 5 has been widely used in metal ion binding studies and antifungal studies[3].
In vitro, Histatin 5 at a concentration of 3200μg/mL for 24 hours was significantly cytotoxic to human gingival fibroblasts and dramatically inhibited cell viability[4]. Treatment of human gingival fibroblasts with 10μg/ml Histatin 5 for 20 minutes inhibited the production of inflammatory cytokines (IL-6 and IL-8) induced by P. gingivalis and lipopolysaccharides[5].
In vivo, Histatin 5 gel at a dose of 100μg/mL three times daily applied to the tongues of mice for three days prevented the occurrence of oral ulcers and significantly inhibited Candida albicans[6]. Administration of Histatin 5 (80μM) to the cornea three times daily for one day promoted wound healing in a mouse corneal injury model[7].
References:
[1] Gusman H, Travis J, Helmerhorst E J, et al. Salivary histatin 5 is an inhibitor of both host and bacterial enzymes implicated in periodontal disease[J]. Infection and immunity, 2001, 69(3): 1402-1408.
[2] Puri S, Edgerton M. How does it kill?: understanding the candidacidal mechanism of salivary histatin 5[J]. Eukaryotic cell, 2014, 13(8): 958-964.
[3] Zolin G V S, Fonseca F H, Zambom C R, et al. Histatin 5 metallopeptides and their potential against Candida albicans pathogenicity and drug resistance[J]. Biomolecules, 2021, 11(8): 1209.
[4] Moffa E B, Mussi M C M, Xiao Y, et al. Histatin 5 inhibits adhesion of C. albicans to reconstructed human oral epithelium[J]. Frontiers in Microbiology, 2015, 6: 885.
[5] Imatani T, Kato T, Minaguchi K, et al. Histatin 5 inhibits inflammatory cytokine induction from human gingival fibroblasts by Porphyromonas gingivalis[J]. Oral microbiology and immunology, 2000, 15(6): 378-382.
[6] Kong E F, Tsui C, Boyce H, et al. Development and in vivo evaluation of a novel histatin-5 bioadhesive hydrogel formulation against oral candidiasis[J]. Antimicrobial agents and chemotherapy, 2016, 60(2): 881-889.
[7] Shah D, Son K N, Kalmodia S, et al. Wound healing properties of histatin-5 and identification of a functional domain required for histatin-5-induced cell migration[J]. Molecular Therapy Methods & Clinical Development, 2020, 17: 709-716.
Histatin 5可抑制基质金属蛋白酶MMP-2和MMP-9的活性,IC50值分别为0.57μM和0.25μM [1]。Histatin 5能通过结合念珠菌的细胞壁蛋白(Ssa1/2)和多糖,显著抑制多种念珠菌的生长,MIC50值为10-20μg/ml[2]。Histatin 5已广泛应用于金属离子结合研究和抗真菌研究[3]。
在体外,使用3200μg/mL浓度的Histatin 5处理人牙龈成纤维细胞 24 小时,可显著诱导细胞毒性并大幅降低细胞活力[4]。以10μg/ml浓度的Histatin 5 处理人牙龈成纤维细胞20分钟,能抑制牙龈卟啉单胞菌和脂多糖诱导的炎症细胞因子(IL-6和IL-8)产生[5]。
在体内,在小鼠舌面涂抹100μg/mL的Histatin 5凝胶(每日3次,连续3天),可预防口腔溃疡的发生并显著抑制白色念珠菌生长[6]。在小鼠角膜损伤模型中,每日3次局部施用80μM的Histatin 5(持续1天),可促进角膜伤口愈合[7]。
















